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- W2017608864 abstract "c-Met is a transmembrane tyrosine kinase that mediates activation of several signaling pathways implicated in aggressive cancer phenotypes. In recent years, research into this area has highlighted c-Met as an attractive cancer drug target, triggering a number of approaches to disrupt aberrant c-Met signaling. Screening efforts identified a unique class of 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one kinase inhibitors, exemplified by 1. Subsequent SAR studies led to the development of 81 (MK-2461), a potent inhibitor of c-Met that was efficacious in preclinical animal models of tumor suppression. In addition, biochemical studies and X-ray analysis have revealed that this unique class of kinase inhibitors binds preferentially to the activated (phosphorylated) form of the kinase. This report details the development of 81 and provides a description of its unique biochemical properties." @default.
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- W2017608864 date "2011-05-24" @default.
- W2017608864 modified "2023-10-11" @default.
- W2017608864 title "Discovery of a 5<i>H</i>-Benzo[4,5]cyclohepta[1,2-<i>b</i>]pyridin-5-one (MK-2461) Inhibitor of c-Met Kinase for the Treatment of Cancer" @default.
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- W2017608864 cites W1987843996 @default.
- W2017608864 cites W1998450601 @default.
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- W2017608864 doi "https://doi.org/10.1021/jm200112k" @default.
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